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Kappa agonists, Opioid receptor ligands, Drugs acting on the nervous system, Cyclobutanes

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Analgesics (3)
Cyclic compounds (3)
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Four-membered rings (3)
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Semisynthetic opioids (2)
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butorphanol (42408-82-2, 58786-99-5)  
Stadol  ·  Butorphanol Tartrate  ·  Stadol NS
Butorphanol (BC 2627) is a morphinan-type synthetic agonist–antagonist opioid analgesic developed by Bristol-Myers. Brand name Stadol was recently discontinued by the manufacturer. It is now only available in its generic formulations, manufactured by Novex, Mylan, Apotex and Ben Venue Laboratories.
nalbuphine (20594-83-6)  
Nubain  ·  Nalbuphine Hydrochloride  ·  EN-2234A
Nalbuphine is a semi-synthetic opioid agonist-antagonist used commercially as an analgesic under a variety of trade names, including Nubain and Manfine.
Xorphanol (77287-89-9)  
Xorphanol (INN) (developmental code name TR-5379 or TR-5379M), also known as xorphanol mesylate (USAN), is an opioid analgesic of the morphinan family that was never marketed. Xorphanol is a mixed agonist–antagonist of opioid receptors, acting preferentially as a high-efficacy partial agonist/near-full agonist of the κ-opioid receptor (Ki = 0.4 nM; EC50 = 3.3 nM; Imax = 49%; IA = 0.84) and to a lesser extent as a partial agonist of the μ-opioid receptor (Ki = 0.25 nM; IC50 = 3.4 nM; Imax = 29%) with lower relative intrinsic activity and marked antagonistic potential (including the ability to antagonize morphine-induced effects and induce opioid withdrawal in opioid-dependent individuals). The drug has also been found to act as an agonist of the δ-opioid receptor (Ki = 1.0 nM; IC50 = 8 nM; Imax = 76%).
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Kappa agonists
Opioid receptor ligands
Drugs acting on the nervous system
Cyclobutanes